Platelets aggregation inhibition

Other papers in the Symposium deal with the antioxidant and hypolipidemic effects of IP6, its chelating effects in heavy metal toxicity, inhibition of renal stones and other beneficial effects such as inhibition of platelet aggregation, inhibition of inflammatory responses (Shamsuddin, 1998). The lipid lowering effect and anti-neoplastic effect of 1P6 were extensively reviewed (Jariwalla, 1999). Hence, 1P6 is a valuable component of rice bran in preventing disease and maintaining health. 1P6 is present at 1.8-2% in rice bran. 

New nitrosothiols are being synthesized and tested for activity. These include structures 1-6 in Section II.A as well as those derived from cysteine residues within proteins. One example of a S-nitrosocysteine within a polypeptide46 is remarkably stable in the solid form, contrasting with the marked instability of S-nitrosocy stein e itself. The S,S dinitrosodithiol 11 has been shown to have platelet aggregation inhibition properties of the same order of magnitude as GTN and vasodilation properties somewhat less than those possessed by GTN17. 

Platelet aggregation inhibition. Methanol extract of the fruit, at a concentration of 500 pg/mL, produced weak activity on human platelets vs collagen-induced... 

The 6- or 7-phenyl-substituted l-ethyl-pyrazino[2,3-r-][l,2,6]thiadiazine 2,2-dioxides 187 were found to show significant platelet aggregation inhibition comparable to other antithrombotic agents. Strong evidence was found that this activity was due to interference with the platelet arachidonic acid pathway <1999JME1698>. 

It is indicated for platelet aggregation inhibition as adjunct to percutaneous transluminal coronary angioplasty or atherectomy (PTCA). 

Interestingly, only the enantiomencally pure (-t-)-clopidogrel (2) exhibits platelet aggregation inhibiting acuvity, while the (-)-(2) is inactive. Moreover, the inactive (-)-... 

Prostacyclin (PGI2) has remarkable antihypertensive and platelet aggregation inhibiting properties. This important compound has been synthesized from the 5,6-djdehydro-PGF2a derivative as outlined in Scheme 8 10b). The unique 2-alkylidenetetrahydrofuran structure is constructed with excellent stereoselectivity (Z E > 33 1) by cyclization of the ace-... 

In the course of another screening for the induction of GST activity in RL34 cells, MS-ITC was inadvertently isolated from wasabi as a potential inducer of GST. MS-ITC administered to rodents also showed both activities in vivo. As a result of elucidation of the platelet aggregation inhibition and the GST induction mechanisms of MS-ITC, the isothiocyanate moiety of MS-ITC plays an important role for antiplatelet and anticancer activities because of its high reactivity with sulfhydryl (RSH) groups in biomolecules (GSH, cysteine residue in a certain protein, etc.) (Figure 42.3). 

Inhibited collagen- and ADP-induced human platelet aggregation inhibited lysolecithin-in-duced K+ efflux from erythrocytes 361,362... 

PGR analog/mimetic (epoprostenol, FR181157) Sildenafil Inhibits platelet aggregation Inhibits type-5 phosphodiesterase and reduces platelet activation... 

MOA Nonselective cyclooxygenase (COX) Inhibitor, inhibits TXAj platelet aggregation. Inhibits ADP platelet receptor. Inhibits ADP platelet receptor. 

ADENOSINE RECEPTOR AGONISTS act extra-cellularly at receptors variously known as adenosine receptors, PI purine receptors, PI receptors, P purinoceptors, or nucleoside receptors. Adenosine receptors have a wide range of mainly inhibitory actions in the body, including cardiac slowing, a fall in blood pressure, dilation of bloqd vessels, inhibition of platelet aggregation, inhibition of intestinal movements and actions within the central nervous system. 

---